Usage of sewage effluent in irrigation of some woody tree seedlings. Part 3: Swietenia mahagoni (L.) Jacq.

A pot experiment was investigated to study the effect of sewage irrigation treatments (primary and secondary effluents) compared with tap water on the growth and chemical constituents of mahogany seedlings (Swietenia mahagoni (L.) Jacq.) as well as soil chemical properties. The experiment was conducted at a greenhouse in the nursery of Timber Trees Research Department of Sabahia, Horticultural Research Station in Alexandria, Egypt, from June 2003 to December 2004 for three irrigation periods (6, 12 and 18 months). The sewage effluent waters were taken from oxidation ponds located in New Borg EL-Arab city and used directly for irrigation.The primary effluent treatment was superior than other treatments in improving the growth parameters (plant height, stem diameter, leaf area, leaves number, fresh and dry weights of leaves, shoots and roots and shoot/root ratio) and showed the highest concentration and total uptake of N, P, K, Cd, Ni, Pb and Fe in plant parts, followed by secondary effluent then tap water. The data revealed that soil salinity in terms of electrical conductivity of saturated paste (EC), CaCO₃%, organic matter% and soluble anions and cations were influenced significantly by primary or secondary effluent treatment. The data also showed that the use of sewage effluent for irrigation increased N, P, K and DTPA-extractable-heavy metals (Cd, Cu, Ni, Pb, Fe, Mn and Zn). The effects of sewage effluent on growth parameters and elements content in plant parts and treated soil were more pronounced as water treatments were used for long period.The results suggested that the use of sewage effluent in irrigating mahogany trees grown on calcareous sandy loam soil was an important agriculture practice for improving soil properties, increasing fuel and timber production, and is an economic and safe way to dispose wastewaters.     

Potent inhibitors of CDK5 derived from roscovitine: Synthesis,biological evaluation and molecular modelling

Cyclin dependent kinase 5 (CDK5) is a serine/threonine kinase belonging to the cyclin dependent kinase (CDK) family. CDK5 is involved in numerous neuronal diseases (including Alzheimer’s or Parkinson’s diseases, stroke, traumatic brain injury), pain signaling and cell migration. In the present Letter, we describe syntheses and biological evaluations of new 2,6,9-trisubstituted purines, structurally related to roscovitine, a promising CDK inhibitor currently in clinical trials (CDK1/Cyclin B, IC₅₀ = 350 nM; CDK5/p25, IC₅₀ = 200 nM). These new molecules were synthesized using an original Buchwald–Hartwig catalytic procedure; several compounds (3j, 3k, 3l, 3e, 4k, 6b, 6c) displayed potent kinase inhibitory potencies against CDK5 (IC₅₀ values ranging from 17 to 50 nM) and showed significant cell death inducing activities (IC₅₀ values ranging from 2 to 9 μM on SH-SY5Y). The docking of the inhibitors into the ATP binding domain of the CDK5 catalytic site highlighted the discriminatory effect of a hydrogen bond involving the CDK5 Lys-89. In addition, the calculated final energy balances for complexation measured for several inhibitors is consistent with the ranking of the IC₅₀ values. Lastly, we observed that several compounds exhibit submicromolar activities against DYRK1A (dual specificity, tyrosine phosphorylation regulated kinase 1A), a kinase involved in Down syndrome and Alzheimer’s disease (3g, 3h, 4m; IC₅₀ values ranging from 300 to 400 nM).     

Chronotype and its relationship with sleep disorders in children with attention deficit hyperactivity disorder

Chronotype can be classified as morningness types, people who prefer morning hours for their physical and mental activities; eveningness types, people who prefer the afternoon or evening hours; and intermediate types, those who show characteristics of both morningness and eveningness types. Attention deficit hyperactivity disorder (ADHD) has been linked with disturbances in chronotype, particularly increased eveningness. Despite the possibility of an association between chronotypes, sleep disturbances and ADHD symptoms, there is little evidence of this association considering the child population. The purpose of this study was to examine chronotype preferences in children aged between 7 and 12 years who were diagnosed as having ADHD in the context of sleep disturbances. The Schedule for Affective Disorders and Schizophrenia for School Age Children-Present and Lifetime Version, Conner’s Rating Scales, Children’s Sleep Habit Questionnaire and Children’s Chronotype Questionnaire were used for the evaluation of children with ADHD and healthy controls. The ADHD group was 73% combined-type, and the eveningness scores of the ADHD group (n = 52) were significantly higher than the control group (n = 52) (p < 0.01). There was a positive correlation between the higher scores of eveningness and total scores on resistance to sleep time (p < 0.09), respiratory problems during sleep and daytime sleepiness in the ADHD group. CSHQ total score was found to be a predictive factor for eveningness among children with ADHD (p < 0.01). These findings highlight possible reciprocal links between ADHD symptoms, sleep disturbances and chronotype in children aged 7–12 years, which might lead to individualized treatment options.     

Slime production and proteinase activity of Candida species isolated from blood samples and the comparison of these activities with minimum inhibitory concentration values of antifungal agents

Slime and proteinase activity of 54 strains consisting of 19 Candida parapsilosis and 35 C. albicans strains isolated from blood samples were investigated in this study. Ketoconazole, amphothericin B, and fluconazole susceptibility of Candida species were compared with slime production and proteinase activity of these species. For both Candida species, no correlation was detected between the slime activity and minimum inhibitory concentration (MIC) values of the three antifungal agents. For both Candida species no correlation was detected between the proteinase activity and the MIC values of amphothericin B, and fluconazole however, statistically significant difference, was determined between the proteinase activity and MIC values of ketoconazole (p = 0.007). Slime production was determined by using modified Christensen macrotube method and proteinase activity was measured by the method of Staib. Antifungal susceptibility was determined through the guidelines of National Committee for Laboratory Standards (NCCLS M27-A).     

Expression of the human FUSED protein in <Emphasis Type="Italic">Drosophila</Emphasis>

The Drosophila segment polarity gene fused, which encodes a serine threonine kinase, is required to transmit the Hedgehog (Hh) signal in imaginal discs. To explore the functional homology between the human protein FUSED (hFU) and the Drosophila protein fused (dFu), we have subjected hFU to a precise and well-defined Hh signalling assay of Drosophila wing development. In the wildtype, hFU affects the expression of Hh target genes leading thus to defects in adult wings. In fu mutants, overexpression of hFU cannot rescue the fu phenotype. These results suggest that hFU in Drosophila interferes with endogenous Hh signalling probably by competing with endogenous dFu when binding its partners but cannot perform the normal Fu function.Edited by C. Desplan     

Anaesthesia and the acute phase protein response in children undergoing circumcision

Concentrations of acute phase proteins (CRP: C-reactive protein, albumin) change during surgery. We investigated the acute phase response to circumcision and the effects of anaesthesia on this response. The children were divided into four groups; group 1 (intratracheal general anaesthesia, n=40), group 2 (general anaesthesia with mask, n=20), group 3 (ketamine, n=20), group 4 (local anaesthesia, n=35). Blood samples were obtained, 24 hours before circumcision, after premedication, and 24 hours after circumcision. CRP and albumin before circumcision were comparable for all groups. There was no increase in CRP, and albumin remained steady throughout the study. No difference was observed among the groups, and related to anaesthesia. No responsiveness may be explained with the size of injured tissue or anatomical and histological type of preputium.     

Synthesis of novel 5-aryl-2-thio-1,3,4-oxadiazoles and the study of their structure-anti-mycobacterial activities

The preparation of novel 5-aryl-2-thio-1,3,4-oxadiazoles 4a-41 and the computer-aided study of their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) are reported. The average accuracy of the electronic-topological method and neural network methods applied to the activity prediction in leave-one-out cross validation is 80%.     

Tripeptides with ionizable side chains adopt a perturbed polyproline II structure in water

The present paper reports the conformations of the acidic and basic homotripeptides triglutamate, triaspartate, and trilysine in aqueous solution to better understand their relevance for the structure of disordered proteins and protein segments and for a variety of protein binding processes. The determination of the dihedral angles of the central amino acid residue was achieved by analyzing the amide I band profile of the respective polarized visible Raman, Fourier transform infrared (FT-IR), and vibrational circular dichroism (VCD) spectra by means of recently developed algorithms [Schweitzer-Stenner, R. (2002) Biophys. J. 83, 523-532; Eker et al. (2002) J. Am. Chem. Soc. 124, 523-532]. The results were validated by measuring the UV electronic circular dichroism (ECD) spectra of the peptides. The analyses revealed that a polyproline II-like conformation is predominant at room temperature. For triaspartate and triglutamate the dihedral angles of phi = -70 degrees, psi = 165 degrees and phi = -60 degrees, psi = 160 degrees were obtained, respectively. A similar conformation, i.e., phi = -50 degrees, psi = 170 degrees, was obtained for trilysine, which is at variance with the earlier reported left-handed turn structure. The ECD spectrum of charged tripeptides displayed symmetric negative and positive couplets at 190 and 210 nm, which are interpreted as indicating a somewhat, perturbed polyproline II conformation, in agreement with the obtained dihedral angles. Comparison with literature data shows that the investigated tripeptides are ideal model systems for understanding the local conformation of functionally relevant K3, K2X, E3, and D3 segments in a variety of different proteins.     

Abeta(1-28) fragment of the amyloid peptide predominantly adopts a polyproline II conformation in an acidic solution

To structurally characterize the nonaggregated state of the amyloid beta peptide, which assembles into the hallmark fibrils of Alzheimer disease, we investigated the conformation of the N-terminal extracellular peptide fragment Abeta(1-28) in D(2)O at acidic pD by utilizing combined FTIR and isotropic and anisotropic Raman spectra measured between 1550 and 1750 cm(-1). Peptide aggregation is avoided under the conditions chosen. The amide I' band was found to exhibit a significant noncoincidence effect in that the first moment of the anisotropic Raman and of the IR band profile appears red-shifted from that of the isotropic Raman scattering. A simulation based on a coupled oscillator model involving all 27 amide I' modes of the peptide reveals that the peptide adopts a predominantly polyproline II conformation. Our results are inconsistent with the notion that the monomeric form of Abeta(1-28) is a totally disordered, random-coil structure. Generally, they underscore the notion that polyproline II is a characteristic motif of the unfolded state of proteins and peptides.